Description
ZT-1a is a potent, non-ATP-competitive and selective SPAK inhibitor. ZT-1a inhibits SPAK activity with IC50s of 44.3, 35.0, 46.7 μM at ATP concentrations of 0.01, 0.1 and 1 mM, respectively.
Product information
CAS Number: 212135-62-1
Molecular Weight: 445.73
Formula: C22H15Cl3N2O2
Chemical Name: 5-chloro-N-{5-chloro-4-[(4-chlorophenyl)(cyano)methyl]-2-methylphenyl}-2-hydroxybenzamide
Smiles: CC1=CC(C(C#N)C2C=CC(Cl)=CC=2)=C(Cl)C=C1NC(=O)C1=CC(Cl)=CC=C1O
InChiKey: RPTKRVXJNWPJLU-UHFFFAOYSA-N
InChi: InChI=1S/C22H15Cl3N2O2/c1-12-8-16(18(11-26)13-2-4-14(23)5-3-13)19(25)10-20(12)27-22(29)17-9-15(24)6-7-21(17)28/h2-10,18,28H,1H3,(H,27,29)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 125 mg/mL (280.44 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
ZT-1a inhibits Na-K-2Cl cotransporter (NKCC1) and stimulates K-Cl cotransporters (KCCs) by decreasing their SPS1-related proline/alanine-rich kinase (SPAK)-dependent phosphorylation. ZT-1a inhibits phosphorylation of NKCC1 p-Thr203/207/212 by 72±5.2% at 1 µM ZT-1a and phosphorylation of KCC sites 1/2 by 65-77% at 3 µM in HEK-293 cells. SPAK phosphorylation at Ser373 is inhibited by 70±3.8% inhibition at 3-10 µM ZT-1a. ZT-1a (10 µM) inhibits NKCC1 but stimulates KCC3 activity.
In Vivo:
ZT-1a (10-100 mg/kg) inhibits SPAK-dependent cation-Cl− cotransporters (CCC) phosphorylation in vivo.
Products are for research use only. Not for human use.
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